盐酸氟桂利嗪两种制剂的生物等效性

目的评价2种盐酸氟桂利嗪制剂人体生物等效性。方法用双周期交叉实验设计,采用液相色谱-质谱-质谱联用法测定了20名健康男性受试者口服盐酸氟桂利嗪口腔崩解片和盐酸氟桂利嗪胶囊后血浆中氟桂利嗪的浓度,绘制了血药质量浓度-时间曲线并计算药动学参数。结果20名受试者口服含盐酸氟桂利嗪20 mg的受试制剂和参比制剂后血浆中氟桂利嗪的tmax分别为(2.7±0.6)和(2.5±0.6)h,ρmax分别为(55.85±20.66)和(56.74±21.40)μg.L-1,t1/2分别为(6.70±2.46)和(6.89±1.98)h,用梯形法计算,AUC0-t分别为(419.0±126.7)和(428.1±175.2)μg.h.L-1,AUC0-∞分别为(465.3±147.8)和(477.0±202.3)μg.h.L-1。以AUC0-t计算,盐酸氟桂利嗪口腔崩解片的相对生物利用度平均为(104.6±22.0)%。结论盐酸氟桂利嗪两制剂生物等效。

Bioequivalence of flunarizine preparations

Objective To study the pharmacokinetics of flunarizine and evaluate the bioequivalence of two flunarizine preparations.Methods Flunarizine tablets and flunarizine capsules were given orally to 20 healthy male volunteers.Flunarizine concentrations in plasma were determined by LC/MS/MS and its plasma concentration-time curves were ploted.Results The main pharmacokinetic parameters of tests and reference preparation were obtained:tmax(2.7±0.6) and(2.5±0.6) h,ρmax(55.85±20.66) and(56.74±21.40) μg·L-1,t1/2(6.70±2.46) and(6.89±1.98) h,AUC0-t(419.0±126.7) and(428.1±175.2) μg·h·L-1,AUC0-∞(465.3±147.8) and(477.0±202.3)μg·h·L-1 respectively.According to AUC0-t,the relative bioavailability of flunarizine tablets was(104.6±22.0)%.Conclusions By ANOVA analysis and two-side t-test showd that the two preparations are bioequivalent.